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Use of ligustrazine phosphate in preparing medicine for treating dilated cardiomyopathy

A technology of dilated cardiomyopathy and ligustrazine phosphate, applied in drug combinations, cardiovascular system diseases, pharmaceutical formulations, etc., to reduce the formation of cardiomyopathy, alleviate irregular hypertrophy, and improve the structure of intercalated discs

Inactive Publication Date: 2011-08-17
INST OF LAB ANIMAL SCI CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004]Ligustrazine (C8H12N2) is a Known chemical monomer in many plants such as Rhizoma Chuanxiong, ligustrazine phosphate (C8H12N2·H3PO4 ·H2O, Tetramethylpyrazine Phosphate, TMPP) and its derivatives, its structure and related biological activities have been reported in relevant textbooks and published literature, but ligustrazine phosphate is used as a preparation The use of drugs for treating dilated cardiomyopathy has not been reported so far

Method used

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  • Use of ligustrazine phosphate in preparing medicine for treating dilated cardiomyopathy
  • Use of ligustrazine phosphate in preparing medicine for treating dilated cardiomyopathy
  • Use of ligustrazine phosphate in preparing medicine for treating dilated cardiomyopathy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] 2. Survival Analysis: The cTnT R141W In the transgenic dilated cardiomyopathy model, individuals died during the breeding process. We recorded the number of animals that died in each group from the beginning of administration to the end of observation. The number of animals that died in the negative control group was 0, and the number of animals that died in the model group was 7. Only 2 animals died in the ligustrazine phosphate group. The results showed that ligustrazine phosphate could reduce the death rate of the model of dilated heart disease.

[0021] Example 2

[0022] Effects of long-term administration of ligustrazine phosphate on cardiac function and configuration of model mice with dilated heart disease (ultrasound):

Embodiment 2

[0024] Table 1 Results of echocardiography after 6 months of drug administration

[0025]

[0026]

[0027] Example 3

[0028] Effects of long-term administration of ligustrazine phosphate on the microstructure of the heart of the model mice with dilated heart disease (HE and Masson staining):

Embodiment 3

[0030] 2. Results: Observed under the light microscope, the myocardial fibers in the model group were unevenly hypertrophied, arranged in disorder, and some cells were vacuolated; the nucleus of the myocardial cells was large, deeply stained, and accompanied by abnormal shapes; there was fibrous tissue hyperplasia in the myocardium. The hypertrophy and arrangement disorder of cardiomyocytes in the ligustrazine phosphate group were significantly improved, and the interstitial collagen fibers were also significantly reduced.

[0031] Example 4

[0032] Effects of long-term administration of ligustrazine phosphate on ultrastructure of left ventricle in model mice with dilated heart disease (electron microscope):

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Abstract

The invention belongs to the medicine field and provides the application of ligustrazine phosphate used for preparing a medicament for curing dilated cardiomyopathy. The ligustrazine phosphate has the following functions of: reducing the death rate of genetic dilated cardiomyopathy, improving the heart function of the dilated cardiomyopathy and relieving the expansion of the left ventricle when the ligustrazine phosphate is used for a long period; relieving the hypertrophy of the myocardial cells of the dilated cardiomyopathy as well as the hyperplasia of interstitial collagen; relieving the uneven thickness of the myocardial fibers, disorderly arrangement, mitochondrial swelling, cristae fragmentation, sarcoplasmic reticulum expansion and damaged intercalated disc connection of the dilated cardiomyopathy; improving the expression of the ligandin Cx40 of the myocardial cells, improving the expression of Myl4 and Myl7 of a myosin light chain, reducing the expression of Myot as well as reducing the expression of collagenous fibers, Col1a1 and Col3a1.

Description

technical field [0001] The invention relates to ligustrazine phosphate, in particular to a new application of ligustrazine phosphate. Background technique [0002] Dilated cardiomyopathy is a myocardial disease mainly characterized by ventricular dilation and impaired myocardial systolic function. The clinical manifestations are progressive heart failure, arrhythmia, thromboembolism, and even sudden death. The prognosis is extremely poor, and the 5-year survival rate Less than 50%. The typical pathological features are dilation of ventricular cavity, thinning of heart wall, and apoptosis of cardiomyocytes. The main etiology is viral myocarditis and gene mutation, accounting for 70% of the incidence of dilated cardiomyopathy. [0003] A variety of mutated genes associated with dilated cardiomyopathy have been found in clinical studies, but most gene mutations can cause HCM and DCM at the same time, while the R141W mutation of cTnT protein (arginine Arg→tryptophan Trp of tro...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4965A61P9/04A61P9/06
Inventor 张连峰赵海萍秦川李万波
Owner INST OF LAB ANIMAL SCI CHINESE ACAD OF MEDICAL SCI
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